Nrf2 signaling activation by a small molecule activator compound 16 inhibits hydrogen peroxide-induced oxidative injury and death in osteoblasts.

ABSTRACT: We explored the potential activity of compound 16 (Cpd16), a novel small molecule Nrf2 activator, in hydrogen peroxide (H₂O₂)-stimulated osteoblasts. In the primary murine/human osteoblasts and MC3T3-E1 murine osteoblastic cells, Cpd16 treatment at micro-molar concentrations caused disassociation of Keap1-Nrf2 and Nrf2 cascade activation. Cpd16 induced stabilization of Nrf2 protein and its nuclear translocation, thereby increasing the antioxidant response elements (ARE) reporter activity and Nrf2 response genes transcription in murine and human osteoblasts. Significantly, Cpd16 mitigated oxidative injury in H₂O₂-stimulited osteoblasts. H₂O₂-provoked apoptosis as well as programmed necrosis in osteoblasts were significantly a

SUBMITTER: Zhao JW 

PROVIDER: S-EPMC9360014 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature